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11. 发明授权

US07115598B2 Substituted 1,4-diazepines and uses thereof 有权
标题翻译：取代的1,4-二氮杂及其用途
公开(公告)号：US07115598B2
公开(公告)日：2006-10-03
申请号：US10829040
申请日：2004-04-21
申请人： Tianbao Lu , Karen L. Milkiewicz , Pierre Raboisson , Maxwell David Cummings , Raul R. Calvo , Daniel J. Parks , Louis V. Lafrance, III , Juan Jose Marugan Sanchez , Joan Gushue , Kristi Leonard
发明人： Tianbao Lu , Karen L. Milkiewicz , Pierre Raboisson , Maxwell David Cummings , Raul R. Calvo , Daniel J. Parks , Louis V. Lafrance, III , Juan Jose Marugan Sanchez , Joan Gushue , Kristi Leonard
IPC分类号： C07D243/14 , A61K31/55
CPC分类号： C07D243/14
摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译：本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R a， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4，或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

12. 发明申请

US20050250771A1 Substituted indoles and their use as integrin antagonists 有权
标题翻译：取代的吲哚及其作为整联蛋白拮抗剂的用途
公开(公告)号：US20050250771A1
公开(公告)日：2005-11-10
申请号：US11005294
申请日：2004-12-06
申请人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
发明人： Tianbo Lu , Bruce Tomczuk , Louis LaFrance , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
IPC分类号： A61K31/404 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/5383 , A61P3/06 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D213/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D498/04 , A61K31/538 , A61K31/405 , A61K31/4745 , A61K31/506 , C07D413/02 , C07D43/02
CPC分类号： C07D213/74 , C07D209/08 , C07D401/12 , C07D401/14 , C07D471/02 , C07D471/04 , C07D471/14
摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, , R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白拮抗剂的新型取代的吲哚化合物，例如阿尔茨海默氏症和/ 整联蛋白，其药学上可接受的盐及其药物组合物。该化合物可用于治疗由α3β3和α5β5 5介导的病理状况。整合素，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。化合物具有以下通式：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8，R 9，R 9， R 10，R 11，R 12，R 12，R 14，D 12，，X，W，a，m，n，i，j，k和v在本文中定义。

13. 发明申请

US20050234081A1 Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效
标题翻译：新型噻吩脒，其组合物和治疗补体介导的疾病和病症的方法
公开(公告)号：US20050234081A1
公开(公告)日：2005-10-20
申请号：US10515554
申请日：2003-05-28
申请人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Hufnagel , Jeremy Travins , Shelley Ballentine , Kenneth Wilson , Maxwell Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen
发明人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Hufnagel , Jeremy Travins , Shelley Ballentine , Kenneth Wilson , Maxwell Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen
IPC分类号： C07D333/22 , A61K31/381 , A61K31/404 , A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4535 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/662 , A61P1/04 , A61P3/10 , A61P5/14 , A61P5/48 , A61P7/00 , A61P7/06 , A61P7/08 , A61P7/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/00 , A61P31/04 , A61P37/00 , A61P37/06 , A61P37/08 , A61P41/00 , A61P43/00 , C07D333/12 , C07D333/38 , C07D333/54 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D495/04 , C07F7/08 , C07F7/10 , C07F9/6553 , C07D49/02
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D495/04 , C07F7/0812 , C07F9/655345
摘要： Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
摘要翻译：公开了一种治疗由补体级联的经典途径介导的急性或慢性病症症状的方法，包括向需要这种治疗的哺乳动物施用治疗有效量的式（I）化合物或溶剂合物，水合物或其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7，在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。

14. 发明申请

US20050209225A1 Substituted indoles and their use as integrin antagonists 审中-公开
标题翻译：取代的吲哚及其作为整联蛋白拮抗剂的用途
公开(公告)号：US20050209225A1
公开(公告)日：2005-09-22
申请号：US11005596
申请日：2004-12-06
申请人： Tianbao Lu , Louis LaFrance , Bruce Tomczuk , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
发明人： Tianbao Lu , Louis LaFrance , Bruce Tomczuk , Thomas Markotan , Juan Marugan Sanchez , Victor Marder , David U'Prichard , Beth Anaclerio , Zihong Guo , Wenzi Pan , Kristi Leonard
IPC分类号： A61K31/404 , A61K31/4375 , A61K31/4439 , A61K31/4709 , A61K31/5383 , A61P3/06 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D213/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D498/04 , A61K31/538 , A61K31/405 , A61K31/4745 , A61K31/506
CPC分类号： C07D213/74 , C07D209/08 , C07D401/12 , C07D401/14 , C07D471/02 , C07D471/04 , C07D471/14
摘要： The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by αvβ3 and αvβ5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis. The compounds have the general formula: where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, D, X, W, a, m, n, i, j, k and v are defined herein.
摘要翻译：本发明涉及作为αV（alphav）整联蛋白的拮抗剂的新的取代的吲哚化合物，例如α缬氨酸和/ β5整联蛋白，其药学上可接受的盐及其药物组合物。该化合物可用于治疗由α3β3和α5β5 5介导的病理状况。整合素，包括肿瘤生长，转移，再狭窄，骨质疏松症，炎症，黄斑变性，糖尿病性视网膜病变和类风湿性关节炎等病症。化合物具有以下通式：其中R 1，R 2，R 3，R 4，R 4， R 5，R 6，R 7，R 8，R 9，R 9， D 10，R 11，R 12，R 13，R 14，D， X，W，a，m，n，i，j，k和v在本文中定义。

15. 发明申请

US20050004031A1 Conjugated complement cascade inhibitors 失效
标题翻译：共轭补体级联抑制剂
公开(公告)号：US20050004031A1
公开(公告)日：2005-01-06
申请号：US10869430
申请日：2004-06-16
申请人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Hufnagel , Shelley Ballentine , Jeremy Travins , Kristi Leonard , Roger Bone
发明人： Nalin Subasinghe , Ehab Khalil , Farah Ali , Heather Hufnagel , Shelley Ballentine , Jeremy Travins , Kristi Leonard , Roger Bone
IPC分类号： A61K47/48 , A61K38/17
CPC分类号： A61K47/60
摘要： The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor.
摘要翻译：本发明涉及缀合的补体级联抑制剂，以及使用缀合的补体级联抑制剂治疗患者的方法。

16. 发明申请

US20070203136A1 TRIAZOLOPYRIDAZINES AS KINASE MODULATORS 有权
标题翻译：三唑吡啶作为激酶调节剂
公开(公告)号：US20070203136A1
公开(公告)日：2007-08-30
申请号：US11612020
申请日：2006-12-18
申请人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
发明人： Tianbao Lu , Richard Alexander , Richard Connors , Maxwell Cummings , Robert Galemmo , Heather Rae Hufnagel , Dana Johnson , Ehab Khalil , Kristi Leonard , Thomas Markotan , Anna Maroney , Jan Sechler , Jeremy Travins , Robert Tuman
IPC分类号： A61K31/503 , A61K31/5377 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的三唑并哒嗪化合物：其中R 1，R 5，R 6，R 7， >，R 8和A如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是c-Met的抑制剂，以及这些化合物用于降低或抑制激酶活性的用途 c-Met在细胞或受试者中的调节，并调节细胞或受试者中的c-Met表达，以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与c-Met有关的障碍的用途。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

17. 发明授权

US07109354B2 Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions 失效
标题翻译：噻吩脒，其组合物和治疗补体介导的疾病和病症的方法
公开(公告)号：US07109354B2
公开(公告)日：2006-09-19
申请号：US10445817
申请日：2003-05-28
申请人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Rae Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , M. Jonathan Rudolph , Hui Huang
发明人： Nalin Subasinghe , Ehab Khalil , Kristi Leonard , Farah Ali , Heather Rae Hufnagel , Jeremy M. Travins , Shelley K. Ballentine , Kenneth T. Wilson , Maxwell D. Cummings , Wenxi Pan , Joan Gushue , Sanath Meegalla , Mark Wall , Jinsheng Chen , M. Jonathan Rudolph , Hui Huang
IPC分类号： C07D333/02 , C07D333/32
CPC分类号： C07D417/12 , C07D333/38 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D495/04 , C07F7/0812 , C07F9/655345
摘要： Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.
摘要翻译：公开了一种治疗由补体级联的经典途径介导的急性或慢性病症症状的方法，其包括向需要这种治疗的哺乳动物施用治疗有效量的式I化合物或溶剂合物，水合物或其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7，在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。

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